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Issue 5, 2012
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Novel potassium N-[(2S,3R,4R,5R)-2,3,4,5,6-pentahydroxylhex-1-yl]-L-amino acid dichloroplatinates(II) with high anti-tumor activity and low side reaction

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Abstract

To discover whether novel anti-tumor platinum agents are capable of selectively accumulating in tumor tissue, three novel potassium N-[(2S,3R,4R,5R)-2,3,4,5,6-pentahydroxylhex-1-yl]-L-amino acid dichloroplatinates(II) were prepared. At a dose of 1.67 μmol kg−1 the in vivo anti-tumor potencies of two of the compounds were higher than that of oxaliplatin. The mortality analysis indicated that these compounds resulted in a 100% survival rate, whereas oxaliplatin lead to an 80% survival rate. The organ damage examination indicated that these compounds induced less damage than oxaliplatin. The platinum accumulation in the organs, blood and bone was significantly lower than that of oxaliplatin treated mice, while the platinum accumulation in the tumor tissue was significantly higher than that of the oxaliplatin treated mice.

Graphical abstract: Novel potassium N-[(2S,3R,4R,5R)-2,3,4,5,6-pentahydroxylhex-1-yl]-l-amino acid dichloroplatinates(II) with high anti-tumor activity and low side reaction

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Publication details

The article was received on 04 Jan 2012, accepted on 12 Mar 2012 and first published on 13 Mar 2012


Article type: Paper
DOI: 10.1039/C2MT00005A
Citation: Metallomics, 2012,4, 441-447

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    Novel potassium N-[(2S,3R,4R,5R)-2,3,4,5,6-pentahydroxylhex-1-yl]-L-amino acid dichloroplatinates(II) with high anti-tumor activity and low side reaction

    Y. Wang, G. Kang, J. Liu, M. Zhao, J. Wu, X. Zhang, Y. Li, X. Zhong, Y. Yang and S. Peng, Metallomics, 2012, 4, 441
    DOI: 10.1039/C2MT00005A

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